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Assay Detail

CHEMBL5583155

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant FGFR3/BAIAP2L1 (unknown origin) transduced in mouse BaF3 cells incubated for 48 hrs by Cell Titer Glo assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Hudkins RL, Allen E, Balcer A, Hoffman ID, Iyer S, Neal M, Nelson KJ, Rideout M, Ye Q, Starrett JH, Patel P, Harris T, Swanson RV, Bensen DC.
J Med Chem (2024) 67 : 16737 -16756
PubMed 39258897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.90 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3828009 LY-2874455 1.0 1 9.70
CHEMBL5594526 1 9.10
CHEMBL5593614 1 8.60
CHEMBL3545376 ERDAFITINIB 4.0 1 8.59
CHEMBL5593800 1 8.49
CHEMBL5589661 1 8.44
CHEMBL5595860 1 8.39
CHEMBL5590027 1 8.28
CHEMBL5591286 1 8.24
CHEMBL5591378 1 8.22
CHEMBL5595732 1 8.22
CHEMBL5592858 1 8.21
CHEMBL5595265 1 8.20
CHEMBL5593851 1 8.19
CHEMBL5594411 1 8.09
CHEMBL5592556 1 8.07
CHEMBL5584069 1 8.06
CHEMBL5593595 1 8.00
CHEMBL5595500 1 7.96
CHEMBL5595947 1 7.96
CHEMBL5595996 1 7.92
CHEMBL5592315 1 7.89
CHEMBL5594702 1 7.89
CHEMBL5590817 1 7.85
CHEMBL5595644 1 7.85
CHEMBL5593620 1 7.80
CHEMBL5592211 1 7.80
CHEMBL5594093 1 7.80
CHEMBL5594121 1 7.77
CHEMBL5594646 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3828009 LY-2874455 IC50 = 0.2 nM 9.70
CHEMBL5594526 IC50 = 0.8 nM 9.10
CHEMBL5593614 IC50 = 2.5 nM 8.60
CHEMBL3545376 ERDAFITINIB IC50 = 2.6 nM 8.59
CHEMBL5593800 IC50 = 3.2 nM 8.49
CHEMBL5589661 IC50 = 3.6 nM 8.44
CHEMBL5595860 IC50 = 4.1 nM 8.39
CHEMBL5590027 IC50 = 5.3 nM 8.28
CHEMBL5591286 IC50 = 5.8 nM 8.24
CHEMBL5591378 IC50 = 6.0 nM 8.22
CHEMBL5595732 IC50 = 6.0 nM 8.22
CHEMBL5592858 IC50 = 6.2 nM 8.21
CHEMBL5595265 IC50 = 6.3 nM 8.20
CHEMBL5593851 IC50 = 6.5 nM 8.19
CHEMBL5594411 IC50 = 8.1 nM 8.09
CHEMBL5592556 IC50 = 8.6 nM 8.07
CHEMBL5584069 IC50 = 8.7 nM 8.06
CHEMBL5593595 IC50 = 10.0 nM 8.00
CHEMBL5595500 IC50 = 11.0 nM 7.96
CHEMBL5595947 IC50 = 11.0 nM 7.96
CHEMBL5595996 IC50 = 12.0 nM 7.92
CHEMBL5594702 IC50 = 13.0 nM 7.89
CHEMBL5592315 IC50 = 13.0 nM 7.89
CHEMBL5590817 IC50 = 14.0 nM 7.85
CHEMBL5595644 IC50 = 14.0 nM 7.85
CHEMBL5593620 IC50 = 16.0 nM 7.80
CHEMBL5592211 IC50 = 16.0 nM 7.80
CHEMBL5594093 IC50 = 16.0 nM 7.80
CHEMBL5594121 IC50 = 17.0 nM 7.77
CHEMBL5594646 IC50 = 18.0 nM 7.75
CHEMBL5583622 IC50 = 22.0 nM 7.66
CHEMBL5595795 IC50 = 23.0 nM 7.64
CHEMBL5594474 IC50 = 26.0 nM 7.58
CHEMBL5594509 IC50 = 30.0 nM 7.52
CHEMBL5594268 IC50 = 30.0 nM 7.52
CHEMBL5594969 IC50 = 36.0 nM 7.44
CHEMBL5590821 IC50 = 38.0 nM 7.42
CHEMBL5595523 IC50 = 40.0 nM 7.40
CHEMBL5584096 IC50 = 48.0 nM 7.32
CHEMBL5594925 IC50 = 48.0 nM 7.32
CHEMBL5592520 IC50 = 97.0 nM 7.01
CHEMBL5594374 IC50 = 110.0 nM 6.96
CHEMBL5593408 IC50 = 133.0 nM 6.88
CHEMBL5593361 IC50 = 179.0 nM 6.75